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Chapter 6
Synthesis of benzodiazepines
New 2,4-disubstituted 1,5-benzodiazepine derivatives containing different
functional groups have been synthesized and screened for their antibacterial activity.
The 2,4-disubstituted 1,5-benzodiazepine derivatives were synthesized by reacting
substituted chalcones synthesized using aldol condensation with o-phenylenediamine
(Figure-19). QSAR studies of synthesized derivatives were performed. 61
Figure-19
A facile and efficient synthesis of 1,5-benzodiazepines with an aryl
sulfonamido substituent at C(3) is described. 1,5-Benzodiazepine, derived from the
condensation of benzene-1,2-diamine and diketene, reacts with an
arylsulfonylisocyanate via an enamine intermediate to produce 1,5-benzodiazepines
good yields (Figure-20). 62
Figure-20
Goswami and Das reports the organo catalyzed one-pot synthesis of
substituted 1,5-benzodiazepinesby condensation of o-phenylenediamine, and 1,3-
dicarbonyl compounds at room temperature or under reflux in the presence of
catalytic amount of L-proline as shown in (Figure-20). 63
Figure-20
Department of Chemistry, Saurashtra University, Rajkot-360005 210